Biological Activity
Non-peptide, melanocortin MC4 receptor antagonist (IC50 values are 320, 810 and 2120 nM for MC4, MC3 and MC5 receptors respectively). Decreases cAMP accumulation in HEK-293 cells expressing the MC4 receptor. Increases food intake and reduces loss of lean body mass in tumor bearing mice. Brain penetrant.
Technical Data
| M. Wt | 413.71 |
| Formula | C18H18BrFN2O.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1706524-94-8 |
| PubChem ID | 90488979 |
| InChI Key | KZUMGPQDDCBFBF-UHFFFAOYSA-N |
| Smiles | BrC1=CC(CCC2=C(F)C=CC=C2C3=NCCN3)=C(OC)C=C1.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.37 | 100 | |
| water | 4.14 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 413.71. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.42 mL | 12.09 mL | 24.17 mL |
| 5 mM | 0.48 mL | 2.42 mL | 4.83 mL |
| 10 mM | 0.24 mL | 1.21 mL | 2.42 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Nicholson et al (2006) Peripheral administration of a melanocortin 4-receptor inverse agonist prevents loss of lean body mass in tumor-bearing mice. J.Pharmacol.Exp.Ther. 317 771 PMID: 16436498
Vos et al (2004) Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model. J.Med.Chem. 47 1602 PMID: 15027849
Tucci et al (2005) Potent and orally active non-peptide antagonists of the human melanocortin-4 receptor based on a series of trans-2-disubstituted cyclohexylpiperazines. Bioorg.Med.Chem.Lett. 15 4389 PMID: 16098742
Keywords: ML 00253764 hydrochloride, supplier, ML00253764, hydrochloride, non-peptide, inverse, agonists, antagonists, melanocortin, MC4, receptors, cachexia, in, vivo, brain, penetrant, Melanocortin, Receptors, Melanocortin, Receptors, Tocris Bioscience
